Abstract: The present invention relates to arylcarbonyl and heteroarylcarbonyl anthranilate compounds that may be useful as anti-fibrotic agents. The present invention also relates to methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment disorders.

Abstract: Disclosed are methods for treating Vascular Leak Syndrome. Further disclosed are methods for treating vascular leakage due to inflammatory diseases, inter alia, sepsis, lupus, irritable bowel disease. Yet further disclosed are methods for treating renal cell carcinoma and melanoma. Still further disclosed are methods for reducing metastasis of malignant cells and/or preventing the proliferation of carcinoma cells via spreading due to vascular leakage.

Abstract: Disclosed are compositions and methods for treating and/or preventing infections in mammals, by administering to a mammal a therapeutically effective amount of at least one defensin-like molecule, e.g., in a composition that includes such molecule. Also disclosed are kits that include such molecules, or compositions that include such molecules, as well as instructions for using such molecules to treat a mammal.

Abstract: The present invention provides novel compounds of Chemical Formula I, a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof, a preparation thereof and a composition for the alleviation, prevention or treatment of osteoporosis, comprising thereof in an effective amount, and a method for alleviating, preventing or treating osteoporosis.

Abstract: The present disclosure relates to compounds effective as human protein tyrosine phosphatase beta (HPTP-?) inhibitors thereby regulating angiogenesis. The present disclosure further relates to compositions comprising said human protein tyrosine phosphatase beta (HPTP-?) inhibitors, and to methods for regulating angiogenesis.

Abstract: The present invention relates to guanidine compounds of the general formula I corresponding enantiomeric, diastereomeric and/or tautomeric forms thereof as well as pharmaceutically acceptable salts thereof. The present compound further relates to the use of guanidine compounds as binding partners for 5-HT5 receptors for the treatment of diseases which are modulated by a 5-HT5 receptor activity, in particular for the treatment of neurodegenerative and neuropsychiatric disorders as well as the associated signs, symptoms and dysfunctions.

Abstract: The invention relates to the field of blood coagulation. Novel oxazolidinone derivatives of the general formula (I) processes for their preparation and their use as medicinally active compounds for the prophylaxis and/or treatment of disorders are described.

Abstract: Vicinal substituted cyclopropyl compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function, for example neurological, neurodegenerative and psychiatric disorders including, but not limited to, those comprising cognitive deficits or schizophrenic symptoms.

Abstract: A method of treating a disease state or condition in humans via topical brainstem afferent stimulation therapy via the administration of a drug to the back of the neck of a human patient at the hairline in close proximity to and under or on the area of skin above the brain stem to provide regional neuro-affective therapy is disclosed.

Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).

Abstract: Pharmaceutical compositions of (R)-pramipexole and methods and kits of using such compositions for the treatment of neurodegenerative diseases, or those related to mitochondrial dysfunction or increased oxidative stress are disclosed.

Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions of compounds of formula (I), methods for using such compounds and compositions, and a process for preparing the compounds.

Abstract: The present invention relates to trans-derivatives of formula wherein R1, R2, R3, and the dotted line are as defined herein and to pharmaceutically acceptable acid addition salts thereof. The compounds of formula I are good inhibitors of the serotonin transporter (SERT inhibitors) and simultaneously, they have good activity on the NK-1 receptor (dual effect). By virtue of their efficacy as SERT inhibitors, the compounds in the present invention are particularly useful for the treatment of CNS disorders and psychotic disorders, in particular in the treatment or prevention of depressive states and/or in the treatment of anxiety.

Abstract: The invention relates generally to novel pharmaceutical methods for the treatment of various conditions. Compositions comprising: at least one phosphodiesterase-5-inhibitor in combination with one or more of the following medications: a selective serotonin reuptake inhibitor; a serotonin-norepinephrine reuptake inhibitor; a cholinesterase inhibitor; a dopamine agonist; or a medication suitable to increase the chemical concentrations of the neurotransmitters, selected from amino acids, monoamines, neuropeptides and other agents capable of primary neurotransmission in the synaptic clefts, and their use for treating a neurodegenerative disease in a subject. The invention also relates to: Compositions comprising: at least one phosphodiesterase-5-inhibitor in combination with one or more of the following medications: a selective serotonin reuptake inhibitor; or a cholinesterase inhibitor, and their use for treating damaged skin in a subject.

Abstract: The present invention provides pharmaceutical compositions containing benzene compound(s) represented by General Formula (1) below and, particularly, LPL-activating compositions for use in hyperlipidemia therapeutic and preventive agents, anti-obesity agents, and the like: wherein R1, R2, R3 and R4 are as defined in the specification.

Abstract: The invention is directed to compounds for selectively inhibiting glycosidases, uses of the compounds and pharmaceutical compositions including the compounds, and methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, and/or accumulation or deficiency of O-GlcNAc.

Abstract: The chronic use of p-adrenergic inverse agonists such as nadolol, carvedilol, and ICI-118,551 provides an improved method for the treatment of mucus hypersecretion in subjects with such mucus hypersecretion. One aspect of a method according to the present invention is a method of preventing or controlling mucus hypersecretion in the respiratory tract comprising administering a therapeutically effective quantity of a p-adrenergic inverse agonist to a subject with mucus hypersecretion or at risk of mucus hypersecretion. The invention further encompasses pharmaceutical compositions comprising the p-adrenergic inverse agonist and the additional compound.

Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is a group of formula A or formula B, and X, R2, R3, R4, R5, R6, Ra and Rb are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist and methods of making the subject compounds.

Abstract: Presently provided are methods for (a) modulating an activity of indoleamine 2,3-dioxygenase comprising contacting an indoleamine 2,3-dioxygenase with a modulation effective amount of a compound as described in one of the aspects described herein; (b) treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression in a subject in need thereof, comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (c) treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (d) enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent and a compound as described in one of the aspects described herein; (e) treating tumor-specific immunosuppression associated with cancer compris

Abstract: The invention relates to N-arylaminomethylenebenzothiophenones of General Formula (I) for use as a drug for the treatment of cardiovascular diseases: wherein E is S, O, or CH2, D is CH or NH, and Ar is a phenyl or naphtyl moiety substituted by an electron-withdrawing group, an unsubstituted heteroaryl residue, or a heteroaryl residue substituted by alkyl or an electron-withdrawing group.

Abstract: Inhibitors of HIV-1 protease and compositions containing them are described. Use of the inhibitors and compositions containing them to treat HIV, AIDS, and AIDS-related diseases is described.

Abstract: Compounds of formula I?: or salts thereof are provided. Pharmaceutical compositions comprising a compound of formula I?, processes for preparing compounds of formula I?, intermediates useful for preparing compounds of formula I? and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal are also provided.

Abstract: Compounds disclosed herein including compounds of formula I?: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.

Abstract: The present invention provides methods for the prevention, treatment and/or amelioration of fibrosis or fibrotic conditions. The present invention further provides small molecule inhibitors of Wnt- and TGF-p-mediated ?-catenin signaling to prevent, treat and/or ameliorate fibrosis or fibrotic conditions. Kits comprising small molecule inhibitors of Wnt- and TGF-p-mediated ?-catenin signaling and methods of identifying small molecule inhibitors of Wnt- and TGF-p-mediated ?-catenin signaling are also provided.

Abstract: An extended release tablet formulation comprising pramipexole or a pharmaceutically acceptable salt thereof in a matrix comprising at least one water swelling polymer other than pregelatinized starch.

Abstract: The present invention relates to reagents and methods for influenza virus detection. These reagents and methods disclosed in the present invention enable simple, rapid, specific and sensitive detection of influenza virus types A and B. These reagents are N-acetylneuraminic acid-firefly luciferin conjugates which can be cleaved by influenza virus neuraminidase.

Abstract: The present invention relates to compounds and methods for imaging and treating Alzheimer's disease or an amyloidosis-associated pathological condition that utilize a novel amyloid imaging tracer for detecting amyloid deposits in a subject suffering from these conditions. In certain embodiments, the invention relates to [N-2[18F]fluoropropyl]-2-(4?-(methylamino)-phenyl)-6-hydroxybenzothiazole (F-18MHT) and dimers thereof.

Abstract: The invention relates to compounds of the formula I in which R1, R2, X, A, B and Y1 to Y4 have the meanings indicated in the claims, and/or a pharmaceutically acceptable salt and/or a prodrug thereof. Because of their properties as inhibitors of chemokine receptors, especially as CXCR2 inhibitors, the compounds of the formula I and the pharmaceutically acceptable salts and prodrugs thereof are suitable for the prevention and treatment of chemokine mediated diseases.

Abstract: A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein: one of R3 and R4 is H, and the other is selected from C1-6-alkyl, C1-6-haloalkyl, C1-6-alkoxy, and C6-12-aralkyl; or R3 and R4 are each independently selected from C1-6-alkyl and halo; R9 is a substituted 5 or 6-membered aryl or heteroaryl group or a 6,5- or 6,6-fused biaryl or heterobiaryl group. Compounds of formula (I) exhibit surprisingly high efficacies for human cathepsin S, excellent selectivity verses other mammalian cathepsins and are useful for treatment of diseases such as rheumatoid arthritis, multiple sclerosis, myasthenia gravis, transplant rejection, diabetes, Sjogrens syndrome, Grave's disease, systemic lupus erythematosis, osteoarthritis, psoriasis, idiopathic thrombocytopenic purpura, allergic rhinitis, asthma, atherosclerosis, obesity, chronic obstructive pulmonary disease and chronic pain.

Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

Abstract: Pulmonary arterial hypertension (PAH) can be prevented in persons susceptible to the diseases and PAH patients can be treated by administering an effective dose of a leukotriene inhibitor. Suitable inhibitors include leukotriene A4 hydrolase (LTA4H) inhibitors, leukotriene B4 receptor (BLT1/BLT2) antagonists, 5-lipoxygenase (5-LO) inhibitors, and 5-lipoxgygenase activating protein (FLAP) inhibitors.

Abstract: The present invention provides methods of identifying compounds that selectively induce an oxidative stress response in a biological sample. The present invention further provides methods of treating a subject having a disease associated with oxidative stress using compounds that selectively induce an oxidative stress response in the subject. The invention further provides methods of selectively inducing an oxidative stress response in a cell.

Abstract: The present invention provides methods of making and using 5-(2-(indol-3-yl)-2-oxoethylidene)-3-phenyl-2-thioxothiazolidin-4-one derivatives having HIV-1 or JSP-1 inhibitory activity.

Abstract: A method for treating hair loss in mammals uses compositions containing prostaglandin F analogs. The compositions can be applied topically to the skin. The compositions can arrest hair loss, reverse hair loss, and promote hair growth.

Abstract: Novel heterocyclic derivatives as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.

Abstract: Pharmaceutical compositions of dexpramipexole and methods of using such compositions for the treatment of ALS are disclosed.

Abstract: The invention relates to the nitrobenzothiazole derivatives of general formula (I): and to the use thereof for treating tuberculosis.

Abstract: The present invention provides a compound of formula (I) in free form or in pharmaceutically acceptable salt form a method for manufacturing the compound of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and pharmaceutical compositions.

Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.

Abstract: Topical formulations and method of using the same are provided. The topical formulation comprises a pyrazolylbenzothiazole derivative of the following formula (1) wherein X, R1, R2, R3 and R4 are described herein.

Abstract: The present patent application concerns new ligands of the H4-receptor of formula (I), their process of preparation and their therapeutic use.

Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

Abstract: Compositions of predetermined amounts of R(+) pramipexole and S(?) pramipexole and methods of using the same, including for the treatment and prevention of Parkinson's disease, are provided.

Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.

Abstract: Disclosed are methods of treating and/or preventing infections in mammals caused by microorganisms, by administering to a mammal a therapeutically effective amount of at least one defensin-like molecule, e.g., in a composition that includes such molecule. Also disclosed are the use of such defensin-like molecules for treating and/or preventing infections in mammals; and kits that may include such molecules, or compositions that include such molecules, as well as instructions for using such molecules to treat a mammal.

Abstract: Modified release pharmaceutical compositions (controlled release, sustained release, and/or extended release) of the R-(+) enantiomer of pramipexole (RPPX) and methods of using such compositions for the treatment of neurodegenerative diseases, or those related to mitochondrial dysfunction or increased oxidative stress are disclosed.

Abstract: A method of treating a glomerular disease selected from the group consisting of mesangial proliferative glomerulonephritis, collapsing glomerulopathy, proliferative lupus nephritis, crescentic glomerulonephritis and membranous nephropathy in a subject comprises administering to the subject an effective amount of a glucosylceramide synthase inhibitor.

Abstract: In one aspect, the present invention provides for a compound of Formula I in which in Formula I, the variables X1, X2a, X2b, X2c, R1, B, L, E, A and the subscript n are as defined herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xL proteins.

Abstract: Pharmaceutical compositions of (R)-pramipexole and methods and kits of using such compositions for the treatment of neurodegenerative diseases, or those related to mitochondrial dysfunction or increased oxidative stress are disclosed.

Abstract: Pharmaceutical compositions that have excellent storage stability even though they include a active component that is susceptible to degradation in an acidic environment are disclosed. The stabilized pharmaceutical composition of the invention includes a ring-opened 7-substituted-3,5-dihydroxyheptanoic or a ring-opened 7-substituted-3,5-dihydroxyheptenoic acid, or a pharmaceutically acceptable salt thereof, as an active component and a stabilizing effective amount of at least one amido-group containing polymeric compound or at least one amino-group containing polymeric compound, or combination thereof; wherein the stabilized pharmaceutical composition does not contain a stabilizing effective amount of another stabilizer or a combination of other stabilizers.